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公开(公告)号：US07410980B2
公开(公告)日：2008-08-12
申请号：US10495437
申请日：2002-11-29
IPC分类号： A61K31/443 , C07D405/12
CPC分类号： A61K31/443 , C07D493/04
摘要： A crystal of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxytax-11-en-13-yl (2R,3S)-3-(tert-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate, which has characteristic peaks at diffraction angles (2θ) of 6.2°, 10.3°, 10.7°, 11.4°, and 12.0° in a powder X-ray diffraction pattern, and a method for preparing the aforementioned crystal, which comprises the step of performing crystallization by using an organic solvent selected from the group consisting of a ketone type solvent, a nitrile type solvent, and a mixture thereof, or a mixture of said organic solvent and water.
摘要翻译： （1S，2S，3R，4S，5R，8R，9S，10R，13S）-4-乙酰氧基-2-苯甲酰氧基-9,10 - [（1S）-2-（二甲基氨基）亚乙二氧基] （2R，3S）-3-（叔丁氧基羰基氨基）-3-（3-氟-2-吡啶基）-2-羟基丙酸酯的20-环氧-1-羟基塔克斯-11-烯-13-基 粉末X射线衍射图中衍射角（2θ）为6.2°，10.3°，10.7°，11.4°和12.0°，以及制备上述晶体的方法，包括通过使用有机物进行结晶的步骤 选自酮类溶剂，腈型溶剂及其混合物的溶剂，或所述有机溶剂和水的混合物。
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公开(公告)号：US20050070579A1
公开(公告)日：2005-03-31
申请号：US10495437
申请日：2002-11-29
IPC分类号： A61K31/443 , A61P35/00 , C07D493/04 , C07D43/02 , A61K31/4433
CPC分类号： A61K31/443 , C07D493/04
摘要： A crystal of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxytax-11-en-13-yl (2R,3S)-3-(tert-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate, which has characteristic peaks at diffraction angles (2θ) of 6.2°, 10.3°, 10.7°, 11.4°, and 12.0° in a powder X-ray diffraction pattern, and a method for preparing the aforementioned crystal, which comprises the step of performing crystallization by using an organic solvent selected from the group consisting of a ketone type solvent, a nitrile type solvent, and a mixture thereof, or a mixture of said organic solvent and water.
摘要翻译： （1S，2S，3R，4S，5R，8R，9S，10R，13S）-4-乙酰氧基-2-苯甲酰氧基-9,10 - [（1S）-2-（二甲基氨基）亚乙二氧基] （2R，3S）-3-（叔丁氧基羰基氨基）-3-（3-氟-2-吡啶基）-2-羟基丙酸酯的20-环氧-1-羟基塔克斯-11-烯-13-基 粉末X射线衍射图中衍射角（2θ）为6.2°，10.3°，10.7°，11.4°和12.0°，以及制备上述晶体的方法，包括通过使用有机物进行结晶的步骤 选自酮类溶剂，腈型溶剂及其混合物的溶剂，或所述有机溶剂和水的混合物。
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公开(公告)号：US20070167630A1
公开(公告)日：2007-07-19
申请号：US11579140
申请日：2005-04-27
IPC分类号： C07D493/02
CPC分类号： C07D213/61 , C07D493/08 , Y02P20/55
摘要： Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds. A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R2 is a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds.
摘要翻译： 衍生物有效和廉价地生产，其可用作口服给药的抗肿瘤化合物。 式（1）的化合物（其中R 1是烷基，烯基，炔基，环烷基，芳基或杂环基; R 2， SUP>是任选具有保护基团的羟基）用碱金属高锰酸盐处理以制备式（2）化合物，其可以是用于口服给药的抗肿瘤化合物的起始材料。
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公开(公告)号：US07678919B2
公开(公告)日：2010-03-16
申请号：US12238070
申请日：2008-09-25
IPC分类号： C07D493/04
CPC分类号： C07D213/61 , C07D493/08 , Y02P20/55
摘要： Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds.A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R2 is a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds.
摘要翻译： 衍生物有效和廉价地生产，其可用作口服给药的抗肿瘤化合物。 式（1）化合物（其中R 1为烷基，烯基，炔基，环烷基，芳基或杂环基; R 2为任选具有保护基的羟基） 碱金属高锰酸盐制备式（2）化合物，其可以是口服给药的抗肿瘤化合物的起始物质。
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公开(公告)号：US07456302B2
公开(公告)日：2008-11-25
申请号：US11579140
申请日：2005-04-27
IPC分类号： C07D305/14
CPC分类号： C07D213/61 , C07D493/08 , Y02P20/55
摘要： Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds.A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R2 is a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds.
摘要翻译： 衍生物有效和廉价地生产，其可用作口服给药的抗肿瘤化合物。 式（1）的化合物（其中R 1是烷基，烯基，炔基，环烷基，芳基或杂环基; R 2， SUP>是任选具有保护基团的羟基）用碱金属高锰酸盐处理以制备式（2）化合物，其可以是用于口服给药的抗肿瘤化合物的起始材料。
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公开(公告)号：US20120053349A1
公开(公告)日：2012-03-01
申请号：US13273360
申请日：2011-10-14
IPC分类号： C07D471/04
CPC分类号： C07D513/04
摘要： The present invention provides an isomer of N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide represented by formula (II) or a salt thereof, or a solvate thereof. Such an isomer or a salt thereof, or a solvate thereof is useful as a standard in a test for inspecting impurities in a pharmaceutical composition containing a compound represented by formula (II) or a salt thereof, or a hydrate thereof. The present invention also relates to a substantially pure compound that is useful as a preventive and/or therapeutic drug for thrombotic diseases, and a pharmaceutical composition containing the substantially pure compound.
摘要翻译： 本发明提供N1-（5-氯吡啶-2-基）-N2 - （（1S，2R，4S）-4 - [（二甲基氨基）羰基] -2 - {[（5-甲基-4- 羰基]氨基}环己基）乙二酰胺或其盐或其溶剂合物。 这种异构体或其盐或其溶剂合物可用作检查含有式（II）表示的化合物或其盐或其水合物的药物组合物中的杂质的试验中的标准。 本发明还涉及可用作血栓性疾病的预防和/或治疗药物的基本上纯的化合物，以及含有基本上纯的化合物的药物组合物。
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